143306-64-3Relevant articles and documents
BICYCLIC PIPERIDINE AND PIPERAZINE DERIVATIVES AS GPCR MODULATORS FOR THE TREATMENT OF OBESITY, DIABETES AND OTHER METABOLIC DISORDERS
-
Page/Page column 64-65, (2010/11/03)
The present invention relates to Bicyclic Piperidine and Piperazine Derivatives, compositions comprising a Bicyclic Piperidine and Piperazine Derivative, and methods of using the Bicyclic Piperidine and Piperazine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.
New classes of potent and bioavailable human renin inhibitors
Remen, L'ubos,Bezencon, Olivier,Richard-Bildstein, Sylvia,Bur, Daniel,Prade, Lars,Corminboeuf, Olivier,Boss, Christoph,Grisostomi, Corinna,Sifferlen, Thierry,Strickner, Panja,Hess, Patrick,Delahaye, Stephane,Treiber, Alexander,Weller, Thomas,Binkert, Christoph,Steiner, Beat,Fischli, Walter
body text, p. 6762 - 6765 (2010/06/12)
New classes of de novo designed renin inhibitors are reported. Some of these compounds display excellent in vitro and in vivo activities toward human renin in a TGR model. The synthesis of these new types of mono- and bicyclic scaffolds are reported, and properties of selected compounds discussed.
AMIDE-SUBSTITUTED ARYL PIPERIDINES
-
Page/Page column 75, (2008/12/05)
Amide-substituted aryl piperidines derivatives of the following Formulas are provided:(Formulas), in which the variables are as described herein. Such compounds may be used to modulate calcitonin gene-related peptide (CGRP) receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CGRP modulation in humans, domesticated companion animals and livestock animals, including headache, such as migraine. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such compounds for receptor localization studies and various in vitro assays.
TETRAHYDROPYRIDINE DERIVATIVES
-
Page/Page column 24-25, (2010/02/11)
The invention relates to novel tetrahydropyridine derivatives and use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin. (I) wherein X and Y represent independently hydrogen, fluorine or a methyl group; X and Y do not represent both hydrogen at the same time or X and Y may together form a cyclopropyl ring; W represents a phenyl or a heteroaryl, the heteroaryl ring being a six-membered and non-fused ring, the phenyl ring and the heteroaryl are substituted with V in position 3 or 4; A and B independently represent-O-;-S-;-SO-or-SO2-; U represents aryl or heteroaryl; T represents-CONR1-;-(CH2)pOCO-;-(CH2)pN(R1)CO-;-(CH2)p N(R1)SO2-;-COO-;-(CH2)pOCONR1-or-(CH2)pN(R2)CONR1-; R1 and R2 independently respresent hydrogen; lower alkyl; lower alkenyl; lower alkynil; cycloalkyl; aryl-lower alkyl, heteroaryl-lower alkyl or cycloalkyl-lower alkyl; Q represents lower alkylene or lower alkenylene; M represents hydrogen; cycloalkyl; aryl; heterocyclyl or heteroaryl: